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The clinical application of triptolide (TPL) in tumor therapy has been greatly limited by its toxicity and inefficient delivery. Herein, a localized and sustained-release thermo-sensitive hydrogel was developed for the intra-tumor administration of TPL. Based on the amphiphilic structure of poly (
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OBJECTIVE： To prepare puerarin microemulsion with phase Ⅰ metabolic regulation （R-PR-ME） and to study pharmacokinetic characteristics of rats in vivo. METHODS： R-PR-ME and Puerarin microemulsion without metabolic regulation （NR-PR-ME） were prepared by Shah method. Pseudo-ternary phase diagram was used to optimize microemulsion formula using drug loading amount as index. The particle size and PDI of microemulsion were characterized by using a laser particle size analyzer. Rats were used as animal models， and HPLC method was used to determine the blood concentration of puerarin before and 5， 10， 15， 20， 30， 45， 60， 90， 120， 180， 240， 360， 480， 600 min after intragastric administration of R-PR-ME， NR-PR-ME and puerarin suspension （PR-SP） at puerarin dosage of 120 mg/kg. The pharmacokinetic parameters were calculated by using DAS 2.0 software. SPSS 19.0 software was used for statistical analysis. The relative bioavailability of R-PR-ME was calculated with NR-PR-ME as reference preparation. RESULTS： The formula of R-PR-ME included that oleoyl polyoxyl-6 glyserides （oil phase）-polysorbate 20 （emulsifier）-glycerides （co-emulsifier） mass ratio of 2 ∶ 4 ∶ 4； drug-loading amount of 67.50 mg/g， particle size was （22.59±0.53） nm （n＝3） and PDI was 0.182±0.017 （n＝3）. The formula of NR-PR-ME included that soybean oil （oil phase）-polysorbate 80 （emulsifier）- glycerol （co-emulsifier） mass ratio of 1 ∶ 4.5 ∶ 4.5， drug-loading amount of 61.32 mg/g， particle size of （15.45±1.06） nm（n＝3） and PDI of 0.156±0.012 （n＝3）. Pharmacokinetic parameters of R-PR-ME， NR-PR-ME and PR-SP included that AUC0-600 min were （134.187±37.152）， （65.145±18.762） and （49.623±12.143） μg·min/mL； cmax were （1.316±0.306）， （1.082±0.294） and （0.425±0.106） μg/mL； MRT were （155.068±33.204）， （100.264±27.683）， （60.524±14.086） min； t1/2β were （365.880±101.250）， （283.280±80.940）， （80.063±21.189） min （n＝6）， respectively. Compared with PR-SP， AUC0-600 min， cmax， MRT and t1/2β of R-PR-ME and NR-PR-ME were increased significantly （P＜0.05 or P＜0.01）. Compared with NR-PR-ME， AUC0-600 min， MRT and t1/2β of R-PR-ME were more higher （P＜0.05）. The relative bioavailability of of R-PR-ME was 205.98％. CONCLUSIONS： R-PR-ME is prepared successfully with high drug-loading amount， and can significantly increase the bioavailability of puerarin in rats， compared with PR-SP and NR-PR-ME.
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OBJECTIVE:To explore the effects of the different compatibility ratios of rutin with quercetin on the pharmacoki-netics of rutin in rats in vivo. METHODS:30 rats were randomly divided into rutin group(rutin-quercetin molar ratio of 4:0,the same below),quercetin group(rutin-quercetin ratio of 0:4),BL1 group(rutin-quercetin ratio of 3:1),BL2 group(rutin-quercetin ratio of 2:2)and BL3 group(rutin-quercetin ratio of 1:3),6 rats in each group,all group was administrated 10 mg/kg(calculat-ed by quercetin core of rutin and quercetin) intragastrically. The blood sample 0.3 mL was respectively taken from tail vein after 0.25,0.5,0.75,1,1.5,2,3,4,6,8,10,12,16,20,24 h of administration,the plasma concentration of quercetin(rutin me-tabolite) was determined by HPLC. DAS 2.0 software was used to calculate the pharmacokinetic parameters. RESULTS:The AUC0-24 h in rutin group,quercetin group,BL1 group,BL2 group and BL3 group were (4.908 ± 0.877),(8.382 ± 3.671), (8.473 ± 0.709),(4.366 ± 2.297),(8.914 ± 2.642)μg·h/L;MRT0-24 h were (9.675 ± 1.359),(3.142 ± 0.489),(3.517 ± 1.128), (3.376 ± 1.046),(4.494 ± 1.653) h;tmax were (5.726 ± 5.645),(1.375 ± 0.703),(1.125 ± 1.438),(1.417 ± 2.300),(1.292 ± 0.954) h;and cmax were (0.609 ± 0.202),(2.341 ± 0.539),(2.425 ± 1.217),(1.464 ± 0.677),(3.325 ± 2.425)μg/L. Compared with rutin group,AUC0-24 h and cmax in quercetin group,BL1 group and BL3 group were significantly increased(P0.05). CONCLUSIONS:Quercetin can inhance the related indexes of rutin in rats in vivo.
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<p><b>OBJECTIVE</b>To develop a quantitative analysis of multi-components by single marker(QAMS) method for simultaneous determination of three coumarins in Angelica dahurica var. formosana, by using one standard substance.</p><p><b>METHOD</b>With imperatorin as internal reference standard, and 2 relative correction factors (RCF) to imperatorin were calculated within certain ranges. Their contents in 20 batches of samples, collected from different areas, were determined by both external standard method and QAMS. The method was evaluated by comparison of the quantitative results between the two methods.</p><p><b>RESULT</b>No significant differences were found in the quantitative results of three coumarins in 20 batches of A. dahurica var. formosana determined by the two methods (RSD < 5%).</p><p><b>CONCLUSION</b>QAMS is feasible and suitable for quality control of A. dahurica var. formosana.</p>